RLY-2608

RLY-2608, an oral, mutant-selective PI3Kα allosteric inhibitor, addresses off-target toxicities of current modulators, currently in Ph. I for HR+/HER2- breast cancer treatment.

Relay Therapeutics to present updated clinical data for RLY-2608 + fulvestrant in PI3Kα-mutated, HR+, HER2- breast cancer at the San Antonio Breast Cancer Symposium on Dec 11, 2024. RLY-2608, a mutant-selective PI3Kα inhibitor, aims to treat over 300,000 patients annually in the U.S.

Allosteric inhibitors targeting PIK3CA offer improved safety over orthosteric inhibitors, with STX-478 showing a 67% disease control rate in advanced solid tumors with PIK3CA mutations. RLY-2608 achieved a 33% objective response rate in PI3Kα-mutated breast cancer, highlighting the potential of allosteric inhibition to overcome resistance and reduce toxicities.

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RLY-2608 plus fulvestrant showed clinically meaningful PFS and a favorable safety profile in heavily pretreated PI3Kα-mutated, HR+/HER2- breast cancer patients, with a median PFS of 9.2 months and an ORR of 33% in those with measurable disease.

RLY-2608, an oral, mutant-selective PI3Kα allosteric inhibitor, addresses off-target toxicities of existing modulators like alpelisib and inavolisib. It is in Phase I for HR+/HER2- breast cancer treatment with fulvestrant.

Relay Therapeutics to lay off 10% of workforce, affecting 30 employees, as part of a streamlining process aimed at saving $50 million annually. The biotech, which had a net loss of $92.2 million in Q2 2024, also announced a clinical trial collaboration with Pfizer and positive interim Phase I/II data for RLY-2608 in metastatic breast cancer.

Relay Therapeutics' experimental breast cancer drug, RLY-2608, delayed tumor growth by 9 months in a trial, shrinking tumors in 75% of participants. The drug, targeting PI3Ka mutations, showed potential to replace existing treatments with less toxicity, prompting Relay to plan a pivotal trial for 2024. The study enrolled 118 patients with PI3Ka-mutated, HR-positive, HER2-negative breast cancer.

RLY-2608, a PI3Kα inhibitor, showed 9.2-month median PFS in heavily pre-treated HR+/HER2- metastatic breast cancer patients, with 33% ORR and favorable tolerability. Plans for a 2L pivotal study in 2025 and triplet combinations with ribociclib and atirmociclib are underway.

Relay Therapeutics to report interim data for RLY-2608 600mg BID + fulvestrant in 2L+, CDK4/6-experienced patients with PI3Kα-mutated, HR+/HER2- metastatic breast cancer on September 9, 2024, at 8am ET. RLY-2608 is an allosteric, pan-mutant, isoform-selective PI3Kα inhibitor designed to overcome limitations of traditional orthosteric inhibitors.